Multifunctional bioactive components eliminated from herbal medicine thanks to multi-target ultrafiltration

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Podophyllum sinense, a popular medicinal plant, has multiple phytochemicals and extensive pharmaceutical activities. Modern pharmacological studies have indicated that P. sinense has remarkable activities, such as anti-proliferative, anti-inflammatory, anti-viral effects, etc. However, the specific functional constituents responsible for anti-proliferative, anti-inflammatory and anti-viral activities remain unknown.

To solve this bottleneck, supervised by Professor GUO Mingquan of the Wuhan Botanical Garden of the Chinese Academy of Sciences, FENG Huixia aimed to uncover the correlations between the potential bioactive components of P. sinense extracts and multiple activities.

Affinity ultrafiltration with topoisomerase I (Topo I), Topo II, cyclooxygenase 2 (COX-2) and angiotensin II converting enzyme (ACE2) coupled with high performance liquid chromatography – the spectrometer of triple quadrupole mass electrospray ionization – mass spectrometry / mass spectrometry The technology was later developed to meet this demand.

Several active ingredients were eliminated, and subsequent in vitro validation experiments indicated that two key compounds, diphyllin and podophyllotoxin, showed a higher rate of inhibition against A549 (non-small cell lung cancer) and HT- 29 (colon cancer) versus 5-fluorouracil and etoposide cells.

Meanwhile, diphylline showed significant COX-2 inhibitory activity with IC50 value at 1.29 ± 0.14 mM compared to indomethacin at 1.22 ± 0.08 mM.

Additionally, several representative components against Topo I, Topo II, COX-2, and ACE2 were also confirmed by molecular docking analysis.

This is the first report to successfully explore the selective inhibitors responsible for its pharmaceutical activities correlated to multiple drug targets of P. sinense, and this study is conducive to the discovery of more novel and curative agents of P. sinense or other medicinal plants.

Relevant results were published in Frontiers in Pharmacology and this study was financially supported by the National Natural Science Foundation of China and the Youth Innovation Promotion Association of CAS.

The multi-component, multi-target network constructs incorporating the potential bioactive components removed with multiple drug targets. (Picture by WBG)

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